[Synthesis and biological evaluation of tetrahydro-beta-carline derivatives].
Kinesin spindle protein (KSP/Eg5) is essential for the formation and maintenance of bipolar spindles during mitosis. Inhibition of this protein leads to cell cycle arrest and apoptosis without interfering other microtubule-dependent processes. Therefore, it is a potential target in cancer therapy. Here, a series of tetrahydro-beta-carboline derivatives 5a - k were synthesized as kinesin spindle protein inhibitor. Their structures were confirmed with 1H NMR, ESI-MS and elemental analysis. The synthesized compounds were evaluated for their inhibition of KSP.
Ruan
Xiu-Qin
XQ
Key Laboratory of Carcinogenesis and Intervention of Jiangsu Province, China Pharmaceutical University, Nanjing 210009, China.
You
Qi-Dong
QD
Yang
Lei
L
Wu
Wu-Tong
WT
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002243:Carbolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D016547:Kinesins / Q000037:antagonists & inhibitors / Q000378:metabolism*; D015394:Molecular Structure
D000970:Antineoplastic Agents; D002243:Carbolines; C470243:KIF11 protein, human; D016547:Kinesins